Biomedical subjects

Y L Janin

Publications and source records attributed to Y L Janin.

3 recordsLinked to original sources

PubMed2003

Peptides with anticancer use or potential.

This review is an attempt to illustrate the diversity of peptides reported for a potential or an established use in cancer therapy. With 612 references, this work aims at covering the patents and publications up to year 2000 with many inroads in years 2001-2002. The peptides are classed according to four categories of effective (or plausible) biological mechanisms of action: receptor-interacting compounds; inhibitors of protein-protein interaction; enzymes inhibitors; nucleic acid-interacting compounds. The fifth group is made of the peptides for which no mechanism of action has been found yet. Incidentally this work provides an overview of many of the modern targets of anticancer research.

Animals↗

PubMed1994

Synthesis and biological properties of new benz[h]isoquinoline derivatives.

In order to determine the importance of the pyrrolic nitrogen atom in a series of suitably substituted gamma-carbolines derivatives for their cytotoxic and antitumor properties, a series of structurally related benz[h]isoquinolines were synthesized. When compared to the "parent" gamma-carbolines, these new compounds showed greatly decreased effects on topoisomerases I and II. Whereas the 8-hydroxylated derivatives retained a significant cytotoxicity, all the new compounds were devoid of antitumor effect in the P388 murine ip-ip system.

Animals↗

PubMed1993

Synthesis and evaluation of new 6-amino-substituted benzo[c]phenanthridine derivatives.

Different 7,8,9,10-tetrahydrobenzo[c]phenanthridin-6(5H)-ones (10a-e) were prepared by using a one-pot procedure which includes the preparation of various 6- and 7-alkoxy-1-naphthylisocyanates from 1-naphthylamines and triphosgene, followed by addition of 1-N-morpholino-1-cyclohexenes, and cyclization of the resulting amides upon heating in the presence of hydrogen chloride. Subsequent aromatization, chlorination, and substitution with (dimethylamino)alkylamines, followed by a demethylation or a selective desisopropylation, allowed us to synthesize the derivatives 6a-i and 7a-h bearing a [(dimethylamino)alkyl]amino side chain at their 6-position. These compounds, as the other analogs 5a-b, were devised to further study the structure-activity relationships in the benzo[c]phenanthridine family of antitumor alkaloids led by fagaronine (1a) and nitidine (1b). Topoisomerases I and II cleavable complex assay and evaluation of the cytotoxicity and antitumor properties were performed. In vitro cytotoxicity (L1210 and Calc 18) shows a relationship between the cytotoxicity of these compounds and their topoisomerase poisoning properties. However, all these compounds were devoid of significant antitumor effect on the P388 murine leukemia system.

Adenocarcinoma↗